Alter, S.a.

Pilar Ortega

Carlos Sunkel

Miguel Fau De Casa-Juana

Jaime Priego

Luis Santos

Fernando Dorrego

Mariano Sanchez-Crespo

Javier Cillero

4-alkyl-1,4-dihydropyridines with activity antagonistic of the PAF-'acether' of formula (I) are described, in which R is a saturated alkyl chain C1-2; R' is a saturated or unsaturated C1-16 lineal, branched or cyclic chain that can be interrupted by an oxygen atom and can also represent a 2-(N-morpholine) ethyl group; n is 2 or 3, X is oxygen, sulphur or SO2; Ar represents an aromatic ring that cannot be phenyl when X=S and n=2. The compounds (I) can be prepared (a) by reaction of (II) with (III) and with (IV); or (b) by reacting (V) with (VI) and (IV); or (c) by reaction of (VII) with (VI). In these formulas the different radicals have the meaning given above. Compounds of formula (I) are used for the treatment of pathologic states and disorders in which the PAF-'acether' participates, being used, for example, in treatment of inflammatory processes, psoriasis, glomerulitis, transplant rejection, acute and chronic bronchitis, bronchial asthma, states of shock and allergies Likewise it is used for the treatment of pathologic states and disorders in which it is necessary to stimulate the cellular immunity such as in immunodeficient syndromes and other situations in which the defense capacity is reduced. ##STR1##

1,4-dihydropyridine compounds with PAF-antagonistic activity

4-alkyl-1,4-dihyropyridines, with PAF-antagonist activity, of formula (I) wherein R is saturated C.sub.1 -C.sub.4, R' is saturated C.sub.1 -C.sub.6 alkyl which may be interrupted by an oxygen atom, or 2-tetrahydrofurfuryl and R.sup.2 is saturated C.sub.1 -C.sub.4 or phenyl, the compound wherein R is methyl, R' is ethyl and R.sup.2 is phenyl remain excluded, are described. The compounds (I) are prepared by: (a) reaction of (II) with (III); (b) reaction of (IV) with (V); (c) reaction of (VI) with (III) and with (VII); (d) reaction of (VIII) with (V) and with (VII); or (e) reaction of (VIII) with (VI) and with (VII) in the presence of ammonia. The compounds (I) are useful due to their antagonist activity of the platelet activating factor. ##STR1##

4-alkyl-1,4-dihydropyridines with PAF-antagonist activity

The present invention refers to new 1,4-dihydropyridines, to their obtention processes and to their use as antithrombotic drugs. Said new 1,4-dihdyropyridines have the following general formula (I) ##STR1## wherein R represents hydrogen or a saturated or unsaturated alkyl group, with a linear or branched chain of 1 to 8 carbon atoms,

1,4-Dihydropiridines and their use as antithrombotic drugs

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Madrid, Spain

Pilar Ortega